US10870846B2 - Cellular high throughput encapsulation for screening or selection - Google Patents
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- US10870846B2 US10870846B2 US14/371,031 US201314371031A US10870846B2 US 10870846 B2 US10870846 B2 US 10870846B2 US 201314371031 A US201314371031 A US 201314371031A US 10870846 B2 US10870846 B2 US 10870846B2
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C40—COMBINATORIAL TECHNOLOGY
- C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
- C40B30/00—Methods of screening libraries
- C40B30/04—Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/10—Processes for the isolation, preparation or purification of DNA or RNA
- C12N15/1034—Isolating an individual clone by screening libraries
- C12N15/1037—Screening libraries presented on the surface of microorganisms, e.g. phage display, E. coli display
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/10—Processes for the isolation, preparation or purification of DNA or RNA
- C12N15/1034—Isolating an individual clone by screening libraries
- C12N15/1058—Directional evolution of libraries, e.g. evolution of libraries is achieved by mutagenesis and screening or selection of mixed population of organisms
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/10—Processes for the isolation, preparation or purification of DNA or RNA
- C12N15/1034—Isolating an individual clone by screening libraries
- C12N15/1068—Template (nucleic acid) mediated chemical library synthesis, e.g. chemical and enzymatical DNA-templated organic molecule synthesis, libraries prepared by non ribosomal polypeptide synthesis [NRPS], DNA/RNA-polymerase mediated polypeptide synthesis
Definitions
- GPCR G protein-coupled receptor
- NT neurotrophic factor
- FACS fluorescence-activated cell sorting
- DDM n-Dodecyl- ⁇ -D-Maltopyranoside
- DM n-Decyl- ⁇ -D-Maltopyranoside
- OG n-Octyl- ⁇ -D-Glucopyranoside
- LbL Layer by Layer
- CHAPS 3[(3-cholamidopropyl)-dimethylammonio]-1-propane sulfonate/N,N-dimethyl-3-sulfo-N[3-[[3 ⁇ ,5 ⁇ ,7 ⁇ ,12 ⁇ )-3,7,12-trihydroxy-24-oxocholan-24-yl]amino]propyl]-1-propanaminium hydroxide
- CHS cholesteryl hemisuccinate Tris salt
- CHESS Cellular High throughput Encapsulation, Solubididimethylammonio]
- alginate is a linear copolymer of (1-4)- ⁇ -D-mannuronate and alpha-L-guluronate.
- Hyaluronic acid is a glycosaminoglycan.
- polyions for practicing the invention include, without being restricted to, poly-L-lysine, carboxymethylcellulose, poly(sodium 4-styrenesulfonate), poly(allylamine hydrochloride), sodium polystyrene sulfonate, poly(styrene)-co-styrene sodium sulfonate (NaPSS), PLGA (polylactic-co-glycolic acid), polyacrylic acid or a water soluble polycationic polymer known for use in the cosmetics industry such as one of the polyquaternium list of compounds (a designation for different polycationic polymers used in the cosmetic industry; see the Wikipedia entry for “polyquaternium”).
- the cationic treatment step precedes the anionic treatment step.
- the initial layer depends on the properties of the template surface.
- the surface of the cell is negatively charged due to the lipopolysaccharide (LPS) comprising the external face of the outer membrane. This makes the cell amenable to initial coating with a positively charged polymer.
- LPS lipopolysaccharide
- the process order can be reversed (i.e. the negatively charged layer is applied first) if a particular cell has a positively charged surface.
- the encapsulation step proceeds over several rounds, repeating the sequence of anionic and cationic coating.
- the cationic treatment step followed by an anionic treatment step may be repeated for example 2, 3, 4, 5, 6, 7, 8, 9 or 10 times, giving rise to ever thicker capsules.
- solubilizing the membrane of said encapsulated cells in a solubilization step, giving rise to a plurality of solubilized compartments comprises the step of exposing said plurality of encapsulated cells to a detergent in aqueous solution.
- the method of the invention comprises
- the solubilized compartments are contacted with a ligand to the target protein, and the ligand bears a detectable label.
- the ligand that is contacted with the solubilized compartments is able to enter the solubilized compartment through the perforation or holes in the cell wall or outer membrane—if any is left—and through the encapsulation coated onto the cell in the encapsulation step, to probe the target protein retained inside the solubilized compartment.
- Non-limiting examples for a ligand to practice the invention are an oligopeptide, an (allosteric) enzyme agonist or antagonist or ion channel agonist or antagonist, receptor agonist or antagonist, inverse agonist, reverse agonist and allosteric modulator.
- the ligand may also be an enzyme substrate or a transition state analogue binding to a variant of the target protein.
- Other non-limiting examples for ligands are specific binding molecules such as antibodies, DARPins (see US20120142611 (A1), incorporated by reference herein), FABs, nanobodies or single chain variable fragments (scFv).
- functional proteins polypeptides
- polypeptides may be used as ligands.
- Cells expressing fumarate reductase or mutated fumarate reductase are encapsulated and the compartments solubilized with detergent.
- Water soluble 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is then added to the solubilized compartments, where it enters the compartment and any active fumarate reductase reduces the MTT to insoluble, purple coloured formazan.
- the formazan precipitate remains inside the solubilized compartment and its presence in particular compartments can be detected and isolated using flow cytometry (FACS).
- the detectable label is a fluorescent dye.
- fluorescent dyes are 4′,6-diamidino-2-phenylindole, dihydrochloride (DAPI), xanthene dyes such as 5- or 6-Carboxyfluorescein (5-FAM and 6-FAM) or Fluorescein, rhodamine dyes such as 5- or 6-Carboxytetramethylrhodamine (5 or 6-TAMRA), or cyanine dyes.
- the selected sequence set is submitted to another round of selection according to the method of the invention.
- the selected sequence set is thus subcloned and transfected into cells anew, and submitted to the sequence of encapsulation step, solubilization step, labelling step, selection step and isolation step, one or several times.
- the repetition may be applied to the selected sequence set of the previous repetition without further manipulation of the selected sequence set.
- the selected sequence set is mutated, for example by error prone PCR (Chen & Arnold, Proc. Nat. Acad. Sci. USA 1993, 90:5618-5622).
- the selected sequence set is subjected to a treatment that deletes sequence tracts, recombines or shuffles sequence tracts between selected sequences, or introduces new sequence tracts randomly.
- a treatment that deletes sequence tracts, recombines or shuffles sequence tracts between selected sequences, or introduces new sequence tracts randomly.
- Such manipulation is equivalent to recombination in a physiological setting and enables larger “leaps” in evolutionary space.
- both point mutation and recombination are combined.
- the selected sequence set is diversified by amplification of said expressed nucleic acid sequences by a process introducing mutations into the amplified sequence, and/or by deletion or insertion of sequence tracts into said expressed nucleic acid sequences, and subsequently, the selected sequence set is submitted to another sequence of encapsulation step, solubilization step, labelling step, selection step and isolation step.
- Identity in the context of the present invention is a single quantitative parameter representing the result of a sequence comparison position by position.
- Methods of sequence comparison are known in the art; the BLAST algorithm available publicly is an example.
- the target protein may be any protein expressed in the cell and retained in the solubilized compartment after encapsulation and solubilization.
- One important non-limiting-example is a G-protein coupled receptor protein.
- Other non-limiting examples include ion channels, enzymes, nuclear receptors, transcription factors and DNA/RNA-binding proteins.
- Other examples for target proteins are specific binding molecules such as antibodies, DARPins, FABs, nanobodies or single chain variable fragments (scFv).
- Small-molecular weight target proteins are retained in the solubilized compartments by fusion to other oligopeptides or proteins to form larger structures (e.g. a triple GFP tag), or by reduction of the effective pore size of the solubilized compartment by an increased number of polymer layers.
- FIG. 2 shows a schematic representation of the LbL encapsulation of E. coli cells and the optimization of this method for the current invention
- E. coli cells were encapsulated by laying down alternate layers of positively charged chitosan polymer and negatively charged alginate.
- the amount of aggregated cells produced during the “Hillberg” LbL process was greatly reduced by the addition of EDTA (+EDTA) to the encapsulation solutions of alginate and chitosan.
- EDTA EDTA
- Reducing the pH of the encapsulation solutions below 7 resulted in stronger capsules that were able to resist detergent treatment.
- FIG. 3 shows the characterization of encapsulated cells.
- GPCR-expressing E. coli cells were encapsulated with 1 layer of chitosan and 1 layer of alginate in triplicate and analyzed with FACS.
- the laser scattering properties of the naked cells allowed the definition of an arbitary gate enclosing 91.4% single cells.
- 60.5% of particles detected in the encapsulated cell sample fell within this gate, with most of the remaining particles exhibiting scattering properties characteristic of larger particles.
- FIG. 6 shows the method used to characterize selected 303 library members.
- FIG. 7 shows the amino acid sequences of highly stable selected 303 library members.
- the amino acid sequences of the selected receptors were aligned with parental rat NTS1, D03 and the high expressing clone C7E02. Locations of the transmembrane helices are indicated with cylinders whereas the number of mutations over D03 are shown in the ⁇ column.
- FIG. 8 shows the selection of detergent stable ADRA1A mutants with CHESS.
- Detergent-stable ADRA1A library members were selected with FACS using 200 nM BODIPY FL prazosin.
- 21 selected clones were expressed individually, solubilized and assayed for ligand binding activity after 3 hours in PBS-E(DCC).
- the top 4 receptors were solubilized in PBS-E(DCC) for 3 h at 20° C. in the absence of ligand. Solubilized receptors were captured from the supernatant with streptavidin paramagnetic beads at 4° C. for 1 h.
- ADRA1ADCCA3 black circles
- ADRA1ADCCG4 grey open squares
- ADRA1ADCCD7 black crosses
- ADRA1ADCCD8 grey open circles coated beads were either treated with 20 nM [ 3 H]prazosin for 1 h before being thermally challenged for 30 min at increasing temperatures or (c) treated with 20 nM [ 3 H]prazosin after heating in the absence of ligand.
- No significant signal could be measured from ADRA1A- or A1A-05-coated beads when the receptors were solubilized in the absence of ligand.
- Parallel measurements were taken for every receptor in the presence of 10 ⁇ M unlabeled prasozin as a competitor to determine the specific fluorescence signal. Data points are plotted as the mean of duplicate measurements, 100% represents the signal measured after heating at 20° C. for 30 min. Error bars indicate the standard error of the mean.
- FIG. 9 shows the amino acid sequences of stable selected ADRA1A library members.
- the amino acid sequences of the selected receptors were aligned with parental ADRA1A and the previously identified high expressing mutant A1A-05. Locations of the transmembrane helices are indicated with cylinders whereas the number of mutations over ADRA1A are shown in the L column.
- the problem to be solved was that the cell would immediately disintegrate when exposed to detergent, thereby homogenizing the whole mixture of receptor mutants and plasmids, rendering the process useless for directed evolution, because the crucial genotype to phenotype linkage would be destroyed.
- the “303 library” is a collection of rNTS1 mutants derived from D03. 30 variable positions in this library were identified from a saturation mutagenesis and high functional expression selection strategy. A further 3 amino acid substitutions were included in this library that have been reported to increase the stability of rNTS1. These 33 variable positions were recombined with wild-type residues to produce a library with a theoretical diversity of 8.6 ⁇ 10 9 individual mutants.
- This library was previously applied to bacterial display to identify high expressing mutants (see Schlinkmann et al., J. Mol. Biol. 2012, 422(3), 414-28).
- CHESS is a novel, rapid method for directly generating GPCRs stable to harsh detergents that are perfectly suited to biophysical analyses and crystallography screens.
- CHESS might allow the direct selection of receptor mutants favoring the binding of G-protein mimetics such as peptides or even the G-proteins themselves, which could potentiate the direct selection of receptors stabilized in active conformations.
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| US11661676B2 (en) | 2012-01-09 | 2023-05-30 | Universität Zürich | Cellular high throughput encapsulation for screening or selection |
| US11788123B2 (en) | 2017-05-26 | 2023-10-17 | President And Fellows Of Harvard College | Systems and methods for high-throughput image-based screening |
| US11959075B2 (en) | 2014-07-30 | 2024-04-16 | President And Fellows Of Harvard College | Systems and methods for determining nucleic acids |
| US12460250B2 (en) | 2018-12-13 | 2025-11-04 | President And Fellows Of Harvard College | Amplification methods and systems for MERFISH and other applications |
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| EP3237908B1 (en) * | 2014-12-22 | 2026-04-22 | Universität Zürich | Directed evolution of membrane proteins in eukaryotic cells with a cell wall |
| CA2997530A1 (en) * | 2015-09-04 | 2017-03-09 | The Scripps Research Institute | Methods for identifying novel antibiotics and related compositions |
| JP2020520455A (ja) * | 2017-05-11 | 2020-07-09 | ザ フローリー インスティテュート オブ ニューロサイエンス アンド メンタル ヘルス | 発現した配列の細胞スクリーニングのための真核細胞の被包 |
| AU2020211622A1 (en) * | 2019-01-25 | 2021-08-19 | The Australian National University | Encapsulated cells |
| WO2021099483A1 (en) | 2019-11-20 | 2021-05-27 | Leadxpro Ag | Method of enabling pooled-library based nucleic acid constructs screening |
| WO2021216789A1 (en) * | 2020-04-21 | 2021-10-28 | University Of Maryland, College Park | System, device, and method for single-cell encapsulation and culture |
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| HK1199061A1 (zh) | 2015-06-19 |
| CN104093838B (zh) | 2016-09-07 |
| HUE032889T2 (hu) | 2017-11-28 |
| WO2013104686A1 (en) | 2013-07-18 |
| DK2802656T3 (en) | 2017-01-16 |
| JP2015503926A (ja) | 2015-02-05 |
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| US20210309992A1 (en) | 2021-10-07 |
| EP2802656A1 (en) | 2014-11-19 |
| EP2612916A1 (en) | 2013-07-10 |
| EP2802656B1 (en) | 2016-10-19 |
| CA2860852C (en) | 2021-01-12 |
| AU2013208951A1 (en) | 2014-08-14 |
| AU2013208951B2 (en) | 2018-02-22 |
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